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Papers of the Week

Papers: 2 Feb 2019 - 8 Feb 2019

Animal Studies, Pharmacology/Drug Development

2019 Jun

Br J Pharmacol



The delta opioid receptor positive allosteric modulator BMS 986187 is a G protein biased allosteric agonist.


Stanczyk AM, Livingston KE, Chang L, Weinberg Z, Puthenveedu M, Traynor JR
Br J Pharmacol. 2019 Jun; 176(11):1649-1663.
PMID: 30710458.


The delta opioid receptor (DOPr) is an emerging target for the management of chronic pain and depression. Studies have highlighted the potential of biased signaling, the preferential activation of one signaling pathway over another downstream of DOPr, to generate a better therapeutic profile. BMS 986187 is a recently discovered positive allosteric modulator (PAM) of the DOPr. Here we ask if BMS 986187 can directly activate the receptor from an allosteric site in the absence of orthosteric ligand and if a signaling bias is generated.